Showing 1-30 of 46 results for "C199"
Nils Ludwig et al.
Purinergic signalling, 16(2), 231-240 (2020-05-23)
Exosomes, small-sized extracellular vesicles, carry components of the purinergic pathway. The production by cells of exosomes carrying this pathway remains poorly understood. Here, we asked whether type 1, 2A, or 2B adenosine receptors (A1Rs, A2ARs, and A2BRs, respectively) expressed by...
Zhan-Guo Gao et al.
Cells, 9(5) (2020-05-16)
Allosteric antagonism by bitopic ligands, as reported for many receptors, is a distinct modulatory mechanism. Although several bitopic A2A adenosine receptor (A2AAR) ligand classes were reported as pharmacological tools, their receptor binding and functional antagonism patterns, i.e., allosteric or competitive...
M Williams et al.
The Journal of pharmacology and experimental therapeutics, 241(2), 415-420 (1987-05-01)
CGS 15943A, a triazoloquinazoline, is a potent and selective adenosine receptor antagonist as assessed by its effects on radioligand binding and adenosine-stimulated adenylate cyclase activity in guinea pig synaptoneurosomes. At the adenosine A-1 receptor labeled with [3H]cyclohexyladenosine, CGS 15943A had...
Trinity J Bivalacqua et al.
American journal of physiology. Regulatory, integrative and comparative physiology, 282(6), R1696-R1709 (2002-05-16)
Hemodynamic responses to adenosine, the A(1) receptor agonists N(6)-cyclopentyladenosine (CPA) and adenosine amine congener (ADAC), and the A(2) receptor agonist 5'-(N-cyclopropyl)-carboxamido-adenosine (CPCA) were investigated in the hindquarter vascular bed of the cat under constant-flow conditions. Injections of adenosine, CPA, ADAC...
Bharath Sunchu et al.
Biochemistry, 51(51), 10137-10146 (2012-12-01)
PriA helicase catalyzes the initial steps of replisome reloading onto repaired DNA replication forks in bacterial DNA replication restart pathways. We have used a high-throughput screen to identify a small molecule inhibitor of PriA-catalyzed duplex DNA unwinding. The compound, CGS...
Myung Ha Yoon et al.
Journal of Korean medical science, 18(2), 255-261 (2003-04-15)
Spinal gabapentin has been known to show the antinociceptive effect. Although several assumptions have been suggested, mechanisms of action of gabapentin have not been clearly established. The present study was undertaken to examine the action mechanisms of gabapentin at the...
Stéphane Le Crom et al.
Journal of neurochemistry, 82(6), 1549-1552 (2002-10-02)
Adenosine is known to modulate dopamine responses in several brain areas. Here, we show that tonic activation of adenosine receptors is able to impede desensitization of D1 dopamine receptors. As measured by cAMP accumulation in transfected COS-7 cells, long-term exposure...
A C Ngai et al.
American journal of physiology. Heart and circulatory physiology, 280(5), H2329-H2335 (2001-04-12)
The purpose of this study was to investigate the receptor subtypes that mediate the dilation of rat intracerebral arterioles elicited by adenosine. Penetrating arterioles were isolated from the rat brain, cannulated with the use of a micropipette system, and luminally...
Chi Ting Leung et al.
Purinergic signalling, 10(3), 465-475 (2014-03-07)
Mast cell degranulation triggers hypersensitivity reactions at the body-environment interface. Adenosine modulates degranulation, but enhancement and inhibition have both been reported. Which of four adenosine receptors (ARs) mediate modulation, and how, remains uncertain. Also uncertain is whether adenosine reaches mast...
Kornkamon Lertsuwan et al.
International journal of molecular sciences, 21(3) (2020-02-06)
Cholangiocarcinoma (CCA) is a lethal disease with increasing incidence worldwide. Previous study showed that CCA was sensitive to adenosine. Thereby, molecular mechanisms of CCA inhibition by adenosine were examined in this study. Our results showed that adenosine inhibited CCA cells...
Petr Potmesil et al.
European journal of pharmacology, 540(1-3), 191-199 (2006-05-31)
Newly developed acyclic nucleoside phosphonates, derivatives of adenine and 2,6-diaminopurine bearing the 2-hydroxy-3-(phosphonomethoxy)propyl (HPMP) moiety at the N9-side chain (i.e., HPMPA and HPMPDAP, respectively) were screened for in vitro immunobiological activity, using mouse resident peritoneal macrophages and splenocytes. Both HPMPA...
Lazaros C Foukas et al.
The Journal of biological chemistry, 277(40), 37124-37130 (2002-07-30)
We investigated the effects of methylxanthines on enzymatic activity of phosphoinositide 3-kinases (PI3Ks). We found that caffeine inhibits the in vitro lipid kinase of class I PI3Ks (IC(50) = 75 microm for p110 delta, 400 microm for p110 alpha and...
Johan-Till Pougnet et al.
Scientific reports, 6, 31836-31836 (2016-09-15)
Plasticity at excitatory synapses can be induced either by synaptic release of glutamate or the release of gliotransmitters such as ATP. Recently, we showed that postsynaptic P2X2 receptors activated by ATP released from astrocytes downregulate synaptic AMPAR, providing a novel...
Jillian G Baker et al.
British journal of pharmacology, 159(4), 772-786 (2010-01-29)
The introduction of fluorescence-based techniques, and in particular the development of fluorescent ligands, has allowed the study of G protein-coupled receptor pharmacology at the single cell and single molecule level. This study evaluated how the physicochemical nature of the linker...
Katelyn E Zulauf et al.
Proceedings of the National Academy of Sciences of the United States of America, 117(47), 29839-29850 (2020-11-11)
Carbapenem-resistant Enterobacteriaceae (CRE) are multidrug-resistant pathogens for which new treatments are desperately needed. Carbapenemases and other types of antibiotic resistance genes are carried almost exclusively on large, low-copy-number plasmids (pCRE). Accordingly, small molecules that efficiently evict pCRE plasmids should restore...
E Ongini et al.
Naunyn-Schmiedeberg's archives of pharmacology, 359(1), 7-10 (1999-02-05)
Three structurally related non-xanthine compounds, CGS 15943, ZM 241385 and SCH 58261, are potent A2A adenosine receptor antagonists and have been used as tools in many pharmacological studies. We have now characterized their affinity and selectivity profile on human adenosine...
A J Szkotak et al.
American journal of physiology. Cell physiology, 281(6), C1991-C2002 (2001-11-08)
The regulatory actions of adenosine on ion channel function are mediated by four distinct membrane receptors. The concentration of adenosine in the vicinity of these receptors is controlled, in part, by inwardly directed nucleoside transport. The purpose of this study...
Y Q Lin et al.
Journal of neurophysiology, 93(5), 2787-2796 (2005-01-14)
Schwann cells, from a variety of sources, are known to possess P2Y purinergic metabotropic receptors. However, it is not known if Schwann cells associated with autonomic nerve terminals possess such receptors and if so whether these receptors are activated by...
Tiago Donatelli Serafim et al.
PLoS neglected tropical diseases, 6(9), e1833-e1833 (2012-10-11)
Leishmania parasites, the causative agent of leishmaniasis, are transmitted through the bite of an infected sand fly. Leishmania parasites present two basic forms known as promastigote and amastigote which, respectively, parasitizes the vector and the mammalian hosts. Infection of the...
A Richter et al.
British journal of pharmacology, 134(2), 343-352 (2001-09-21)
1. Recent studies have shown beneficial effects of an adenosine A(2A) receptor agonist in dt(sz) mutant hamsters, an animal model of paroxysmal dystonia, in which stress and consumption of coffee can precipitate dystonic attacks. This prompted us to examine the...
K T Lu et al.
The Chinese journal of physiology, 42(4), 249-253 (2000-03-09)
Caffeine which is present in soft drinks has been shown to increase alertness and allays drowsiness and fatigue. The aim of this study is to investigate whether caffeine could produce a long-term effect on the synaptic transmission using extracellular recording...
Bishop F Hague et al.
Virus research, 93(1), 31-39 (2003-05-03)
A flow cytometric assay that measures binding of human T-lymphotropic virus type 1 (HTLV-1) virions to target cells was used to investigate the binding process and to screen for compounds affecting viral binding. Results showed that adenosine receptor type 2...
Hyung Gon Lee et al.
Yonsei medical journal, 51(6), 960-964 (2010-09-30)
The phosphodiesterase 5 inhibitor sildenafil has antinociceptive effects, mediated by an increase in cGMP. This study examined the role of spinal adenosine and serotonin receptors played in the antinociceptive effects of intrathecal sildenafil. Intrathecal catheters were inserted into the subarachnoid...
John R Fozard et al.
European journal of pharmacology, 475(1-3), 79-84 (2003-09-05)
We have sought evidence for species differences between adenosine A2B receptors by comparing the potencies of eight adenosine receptor antagonists, representing four different chemical classes, at the native adenosine A2B receptors which mediate relaxation of smooth muscle from rat colon...
Thanaporn Kaewphaleuk et al.
Life sciences, 228, 21-29 (2019-04-27)
Ethanol is known to induce NO release and coronary vasorelaxation. Evidence suggests that K+ channels, especially a Ca2+-activated K+ channel (KCa), may regulate endothelial NO production. We aimed to investigate the ethanol effect on K+ currents in human coronary artery...
Fabrizio Vincenzi et al.
Cells, 9(5) (2020-05-24)
Glutamate cytotoxicity is implicated in neuronal death in different neurological disorders including stroke, traumatic brain injury, and neurodegenerative diseases. Adenosine is a nucleoside that plays an important role in modulating neuronal activity and its receptors have been identified as promising...
Petra Ondrackova et al.
Veterinary immunology and immunopathology, 145(1-2), 332-339 (2012-01-10)
Adenosine is a well described anti-inflammatory modulator of immune responses. The aim of the present study was to describe the role of common adenosine agonist 5'-N-ethylcarboxamidoadenosine (NECA) in cytokine production by main porcine T cell subpopulations. TNF-α, IFN-γ, IL-2 and...
John W Phillis et al.
European journal of pharmacology, 476(3), 211-219 (2003-09-13)
The role of adenosine in the cerebrovascular response to carbon dioxide inhalation was evaluated in two sets of experiments. The pial circulation was recorded by a Laser-Doppler flow probe placed over a closed cranial window in methoxyflurane anesthetized rats. Topical...
Yong Qi Lin et al.
Neuroreport, 17(5), 531-535 (2006-03-18)
Schwann cells at the somatic neuromuscular junction possess adenosine receptors that when activated by the release of endogenous transmitter modulate quantal transmitter release. Recently, purinergic receptors have been shown to exist on Schwann cells of axon varicosities in visceral smooth...
Elise M Weerts et al.
Psychopharmacology, 168(1-2), 155-163 (2003-04-02)
Caffeine and the adenosine A(1) and A(2A) receptor antagonist CGS15943 produce many behavioral effects that are similar to those produced by classic stimulant drugs (e.g. cocaine and amphetamines). The current study evaluated whether CGS15943 would maintain self-administration and reinstate extinguished...

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